Vinpocetine

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT VINCETIN (VINPOCETIN)

Composition:

Active ingredient: vinpocetine;

1 tablet contains vinpocetine (calculated as 100 % substance) – 5 mg or 10 mg;

Excipients: lactose monohydrate, microcrystalline cellulose, potato starch, colloidal anhydrous silicon dioxide, macrogol 4000 (polyethylene glycol 4000), magnesium stearate, sodium croscarmellose.

Pharmaceutical form. Tablets.

Main physicochemical properties: white to off-white tablets, flat cylindrical in shape with a bevelled edge. Marbling on the tablet surface is permissible.

Pharmacotherapeutic group.

Psychostimulants and nootropic agents. Vinpocetine.

ATC code: N06BX18.

Pharmacological Properties

Pharmacodynamics

Vinpocetine improves cerebral circulation and brain metabolism, enhancing the brain's tolerance to ischemia. This effect is achieved through a complex mechanism of action. It selectively and significantly enhances cerebral blood flow and the cerebral fraction of cardiac output, reduces resistance in cerebral blood vessels, without affecting systemic circulation parameters (arterial pressure, cardiac output, pulse rate, total peripheral vascular resistance). It primarily enhances blood supply to the ischemic area of the brain without causing a "steal" phenomenon, while blood flow to healthy brain areas remains unchanged. It improves microcirculation in the brain, inhibits platelet aggregation, reduces elevated blood viscosity, increases erythrocyte elasticity, and blocks adenosine uptake by erythrocytes. Vinpocetine enhances brain cells' tolerance to hypoxia, promoting oxygen delivery to tissues. It enhances glucose uptake and metabolism, shifting it toward the more energetically favorable aerobic pathway, and stimulates anaerobic glucose metabolism by inhibiting phosphodiesterase and activating adenylate cyclase, leading to increased concentrations of cAMP and catecholamines in the brain.

Pharmacokinetics

After oral administration, vinpocetine is rapidly absorbed from the gastrointestinal tract; bioavailability is approximately 70%. Maximum plasma concentration is reached within 1 hour. It readily penetrates histohematic barriers, including the blood-brain barrier. It is metabolized in the liver, forming several metabolites, the main ones being apovincaminic acid and hydroxyvinpocetine, both of which possess pharmacological activity. Excretion occurs via urine and bile, primarily as metabolites conjugated with glucuronic acid. The elimination half-life is up to 5 hours.

Clinical characteristics.

Indications.

Neurology. For the treatment of various forms of cerebrovascular pathology: conditions following stroke (cerebral circulation disorder), vertebrobasilar insufficiency, vascular dementia, cerebral atherosclerosis, post-traumatic and hypertensive encephalopathy. Helps reduce psychological and neurological symptoms in cerebrovascular pathology.

Ophthalmology. For the treatment of chronic vascular pathology of the choroid and retina.

Otorhinolaryngology. For the treatment of age-related sensorineural hearing loss, Ménière's disease, and tinnitus.

Contraindications.

Pregnancy or breastfeeding period.

Hypersensitivity to the active substance or to any of the excipients.

The use of the medicinal product in children is contraindicated (due to lack of data from appropriate clinical studies).

Interaction with other medicinal products and other forms of interaction.

During clinical studies, no interactions were observed when vinpocetine was administered concomitantly with beta-blockers such as chloranolol and pindolol, as well as with clomipramide, glyburide, digoxin, acenocoumarol, or hydrochlorothiazide. In isolated cases, an additional effect was observed when alpha-methyldopa and vinpocetine were used concomitantly; therefore, regular monitoring of arterial pressure is required when this combination of medicinal products is used.

Although clinical study data have not confirmed interactions, caution is recommended when vinpocetine is used concomitantly with medicinal products affecting the central nervous system, as well as during concomitant antiarrhythmic and anticoagulant therapy.

Special precautions for use

In cases of increased intracranial pressure, when administering antiarrhythmic agents, or in the presence of arrhythmias and long QT interval syndrome, this medicinal product should be used only after careful assessment of the benefit-risk ratio of therapy.

ECG monitoring is recommended in patients with long QT interval syndrome or when this medicinal product is used concomitantly with other medicinal products that may prolong the QT interval.

This medicinal product contains lactose monohydrate. Patients with rare hereditary disorders such as galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicinal product (one 5 mg Vinpocetine tablet contains 67.3 mg of lactose, and one 10 mg tablet contains 134.6 mg of lactose).

Fertility. No effect on fertility has been observed.

Teratogenicity. No teratogenic effects have been observed.

Mutagenicity. Vinpocetine has no mutagenic effect.

Carcinogenicity. Vinpocetine has no carcinogenic effect.

Use during pregnancy or breastfeeding.

The use of vinpocetine during pregnancy or breastfeeding is contraindicated.

Pregnancy. Vinpocetine crosses the placental barrier but is found in lower concentrations in the placenta and fetal blood than in maternal blood. No teratogenic or embryotoxic effects have been observed. In animal studies, administration of high doses of vinpocetine was associated in some cases with placental hemorrhage and abortion, primarily due to enhanced placental blood flow.

Breastfeeding. Vinpocetine is excreted into breast milk. In studies using radiolabeled vinpocetine, radioactivity in breast milk was 10 times higher than in maternal blood. The amount excreted into breast milk within one hour amounts to 0.25% of the administered dose. Since vinpocetine passes into breast milk and there is no data available on its effects on newborns, the use of vinpocetine during breastfeeding is contraindicated.

Ability to affect reaction speed when driving or operating machinery.

Studies on the influence of vinpocetine on the ability to drive or operate machinery have not been conducted. However, the possibility of somnolence, dizziness, and vertigo occurring during treatment should be taken into account.

Dosage and Administration.

The usual dosage of the medicinal product is 5–10 mg three times daily (15–30 mg daily). Tablets should be taken after meals.

No special dose adjustment is required for patients with renal or hepatic impairment.

The duration of treatment is determined individually by the physician.

Children.

Vinpocetine is contraindicated in children (due to lack of relevant clinical data).

Overdose.

No cases of overdose have been reported. Long-term administration of vinpocetine at a daily dose of 60 mg is also safe. Even a single oral intake of 360 mg of vinpocetine did not cause any clinically significant adverse effects on the cardiovascular system or other effects.

Adverse reactions.

Vinpocetine is a safe medicinal product, as confirmed by safety assessment studies that included data from tens of thousands of patients and demonstrated that even the most frequently occurring adverse effects did not fall into the category of "Common" (>1/100) according to MedDRA definitions. Therefore, the incidence of adverse reactions with the highest probability of occurrence was recorded at less than 1%. For this reason, the "Common" frequency category is absent from the table below.

The adverse reactions listed below are categorized by system organ classes and are presented with their frequencies according to MedDRA terminology:

Shelf life.

2 years.

Do not use after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

10 tablets in a blister; 5 mg tablets № 10x3, № 10x5 in a pack; 10 mg tablets № 10×3.

Prescription status.

Prescription only.

Manufacturer.

JSC "CHEMICAL PHARMACEUTICAL PLANT "CHERVONA ZIRKA".

Manufacturer's location and address of the place of business activity.

1, Gordienkovskaya Street, Kharkiv, Kharkiv region, 61010, Ukraine.